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ID: ALA1147716
Journal: Bioorg Med Chem Lett
Title: A series of 5-aminosubstituted 4-fluorobenzyl-8-hydroxy-[1,6]naphthyridine-7-carboxamide HIV-1 integrase inhibitors.
Authors: Guare JP, Wai JS, Gomez RP, Anthony NJ, Jolly SM, Cortes AR, Vacca JP, Felock PJ, Stillmock KA, Schleif WA, Moyer G, Gabryelski LJ, Jin L, Chen IW, Hazuda DJ, Young SD.
Abstract: A series of 5-amino derivatives of 8-hydroxy[1,6]-naphthyridine-7-carboxamide exhibiting sub-micromolar potency against replication of HIV-1 in cell culture was identified. One of these analogs, compound 12, displayed excellent pharmacokinetic properties when dosed orally in rats and in monkeys. This compound was demonstrated to be efficacious against replication of simian-human immunodeficiency virus (SHIV) 89.6P in infected rhesus macaques.
CiteXplore: 16554152